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Principles > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

define pharmacodynamics

A

what a drug does to the body

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2
Q

define pharmacokinetics

A

what the body does to a drug

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3
Q

define a drug

A

any single synthetic or natural substance of known structure used in treatment, prevention or diagnosis of a disease

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4
Q

define a medicine

A

chemical preparation containing one, or more, drugs used with the intention of causing a therapeutic effect.

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5
Q

examples of regulatory proteins that drugs act on?

A

enzymes, carrier molecules (transporters and pumps), ion channels and receptors

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6
Q

define an agonist

A

a drug that binds to a receptor to produce a cellular response e.g. adrenaline

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7
Q

define an antagonist

A

a drug that reduces or blocks the actions of an agonist by binding to the same receptors e.g. beta blockers

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8
Q

define affinity of an agonist

A

strength and association between a ligand and receptor

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9
Q

define efficacy of an agonist

A

ability of an agonist to evoke a cellular response

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10
Q

do antagonists possess affinity and efficacy?

A

only affinity

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11
Q

define EC50

A

the concentration of an agonist that elicits a half maximal response

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12
Q

same EC50

A

equipotent

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13
Q

what type of competition occurs between agonists and antagonists?

A

competitive inhibition if they bind to the same site, but different site is non-competitive

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14
Q

non-competitive inhibition causes the curve to?

A

not reach max

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15
Q

competitive inhibition causes the curve to

A

shift to the right

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16
Q

receptors are targets of?

A

neurotransmitters,hormones, therapeutic agents

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17
Q

three different ways of chemical signalling

A
  1. autocrine
  2. paracrine
  3. endocrine
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18
Q

four main types of receptors

A
  1. ligand-gated ion channel
  2. G protein-coupled receptor
  3. kinase-linked receptor
  4. nuclear receptors
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19
Q

structure of a ligand-gated ion channel

A

separate glycoprotein subunits with binding sites

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20
Q

which receptors are involved in second messengers?

A

G protein-coupled receptors

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21
Q

structure of G protein-coupled receptors

A

integral membrane protein. single polypeptide with NH2 and COOH, 7 transmembrane alpha-helical spans joined by 3 intracellular and 3 extracellular loops

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22
Q

structure of G-protein

A

peripheral membrane protein with 3 polypeptide subunits (alpha, beta and gamma). Guanine binding site on the alpha subunit that holds GTP or GDP

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23
Q

how is the G protein coupled receptor activated?

A

binding of the agonist

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24
Q

how is the G protein activated

A

the activation of the G-protein coupled receptor causes conformational change in the alpha subunit of the G-protein

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25
Q

what three changes happen to the G-protein to make it activated?

A
  1. G-protein couples with receptor
  2. releases GDP and GTP binds
  3. subunit dissociation
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26
Q

how do you turn off the signal even when the agonist has dissociated?

A

alpha subunit acts as an enzyme hydrolysing GTP to GDP. Subunit recombination.

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27
Q

explain signalling via receptor kinases

A

binding causes autophosphorylation and recruitment of proteins

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28
Q

explain nuclear receptors

A

steroid hormones diffuse across the plasma membrane and combine with an intracellular receptor which moves to the nucleus which switches genes on or off

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29
Q

four fates of drugs in the body

A
  1. Absorption
  2. Distribution
  3. metabolism
  4. excretion
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30
Q

what is metabolism and excretion collectively called?

A

elimination

31
Q

four factors that affect drug absorption

A
  1. solubility
  2. chemical stability (destroyed by acid, etc.)
  3. lipid to water partition coefficient (ability to diffuse across the membrane)
  4. degree of ionisation
32
Q

define pKa

A

pH when 50% of the drug is ionised

33
Q

where are weak acids absorbed

A

stomach lumen, but also small intestine

34
Q

where are bases absorbed

A

small intestine

35
Q

do acidic drugs become less ionised in acid environments

A

yes

36
Q

factors affecting GI absorption are?

A
  • GI motility (rate of stomach emptying)
  • pH at absorption site
  • blood flow
  • way the tablet is manufactured (capsule)
  • presence of transporters
37
Q

advantages of oral administration

A

simple, convenient, non-sterile

38
Q

disadvantages of oral administration

A

inactivation by enzymes and acid, variable absorption

39
Q

define oral availability

A

fraction of drug that reaches systemic circulation after oral ingestion

40
Q

define systemic circulation

A

fraction of drug that reaches systemic circulation after absorption

41
Q

advantages of sublingual administration

A

rapid absorption

42
Q

disadvantages of sublingual route

A

infrequent, few preparations available

43
Q

advantages of rectal administration

A

useful when oral route compromised

44
Q

disadvantages of rectal administration

A

infrequent, variable absorption

45
Q

advantages intravenous

A

rapid onset

46
Q

disadvantages of intravenous

A

sterile preparation required, risk of sepsis

47
Q

advantages of intramuscular

A

rapid onset

48
Q

disadvantages of intramuscular

A

painful

49
Q

which free drugs can move between compartments in the body?

A

ionised and unionised drugs that are not bound to plasma proteins

50
Q

volume of distribution equation

A

dose / plasma concentration

51
Q

define drug clearance

A

the volume of plasma cleared of drug per unit of time

52
Q

clearance determines the?

A

dose rate

53
Q

define chemical equivalence

A

the drug product contains the same amount of active compound

54
Q

define volume of distribution

A

the volume into which a drug appears to be distributed with a concentration equal to that of plasma

55
Q

what is different about a loading dose?

A

it is an initial higher dose before dropping down.

56
Q

define xenobiotics

A

foreign chemicals

57
Q

five things drug metabolism can do

A
  1. convert parent drug to a more polar form
  2. convert it to a less pharmacologically active form
  3. convert inactive to an active form
  4. unchanged activity
  5. change spectrum of action
58
Q

describe phase 1 of drug metabolism

A

makes drugs more polar, adds a chemically reactive group, permits conjugation. Serve as a point of attack for phase 2

59
Q

describe phase 2 of drug metabolism

A

adds an endogenous compound increasing polarity

60
Q

where do phase 1 reactions take place

A

liver

61
Q

what proteins carry out phase 1

A

CYP450

62
Q

what are CYP450’s

A

ahem proteins located on the ER of liver hepatocytes

63
Q

describe the three stages of the P450 cycle

A
  1. drugs enter the cycle
  2. O2 provides two atoms of oxygen
  3. one oxygen forms water and the other oxygen forms a hydroxyl product
64
Q

what does phase 2 usually result in?

A

inactive products

65
Q

define glucuronidation

A

transfer of glucuronic acid

66
Q

three processes carried out by the kidneys in drug excretion

A
  1. glomerular filtration
  2. active tubular secretion
  3. passive reabsorption by diffusion
67
Q

what happens in glomerular filtration?

A

many drugs bind reversibly to large plasma proteins. Only unbound drugs can enter the filtrate.

68
Q

what are the two transporter systems that secrete drugs into the lumen of the nephron?

A
  1. organic anion transporter

2. organic cation transporter

69
Q

describe the organic anion transporter

A

organic anions enter the cell by diffusion or in exchange for alpha-KG. At the apical membrane OA- enters

70
Q

describe the organic cation transporter

A

organic cations enter by diffusion and enter via the apical membrane

71
Q

factors influencing tubular reabsorption are

A
  1. lipid solubility
  2. polarity
  3. urinary flow rate
  4. urinary pH
72
Q

what is Ke

A

elimination rate

73
Q

define elimination rate

A

amount of drug eliminated per unit of time

Principles (11 decks)

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